Uses
4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)benzenamine is a non-competitive AMPA receptor antagonist and was found to have therapeutic potential for cocaine addiction treatment.
Definition
ChEBI: GYKI 52466 is a benzodiazepine.
Biological Activity
Selective non-competitive AMPA receptor antagonist (IC 50 values are 10-20, ~ 450 and >> 50 μ M for AMPA- , kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant. Has anti-proliferative effects in transformed cells. Also available as part of the AMPA Receptor Tocriset™ . Also available as part of the Kainate Receptor Tocriset™ .
in vivo
GYKI 52466 (intraperitoneal injection; 1.76-13.2 mg/kg; once) treatment provides potent anticonvulsant protection against sound-induced seizures in DBA/2 mice[2].
| Animal Model: | Male and female DBA/2 mice tested for sound-induced seizure responses[2] |
| Dosage: | 1.76-13.2 mg/kg |
| Administration: | Intraperitoneal injection; 1.76-13.2 mg/kg; once |
| Result: | Observed Maximal anticonvulsant protection after the i.p. treatment (5-15 min ). |
IC 50
Kainate Receptor: 11 μM (IC
50)
storage
room temperature (desiccate)
